Rac-6β-((ξ)-2-Benzyloxycarbonyl-2-Thiophen-3-Yl-Acetylamino)-6α-Methoxy-Penicillanic Acid Benzyl Ester置于palladium On Activated Charcoal 氢气,碳酸氢钠体系中,用 甲醇,水 作为反应溶剂,化学反应生成 替莫西林 参考文献:Bentley,P.H. Et Al.,Journal Of The Chemical Society. Perkin Transactions I,1979,P. 2455-2467 标题:Bentley,P.H. Et Al.,Journal Of The Chemical Society. Perkin Transactions I,1979,P. 2455-2467
专利号:US-2024197774-A1 优先权日:2021-04-16 标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles 发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO 权利人:UNIV TEXAS 摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-10443047-B2 优先权日:2014-05-01 标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase 发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E 权利人:NOVOGY INC 摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.
专利号:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:US-8399502-B2 优先权日:2008-09-17 标 题 :Analogs of indole-3-carbinol and their use as agents against infection 发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN 权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT 摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
1: Alexandre K, Fantin B. Pharmacokinetics and Pharmacodynamics of Temocillin. Clin Pharmacokinet. 2018 Mar;57(3):287-296. doi: 10.1007/s40262-017-0584-7. 27(12):609-617. French. doi: 10.1016/j.purol.2017.07.242. Epub 2017 Aug 30. 14:81-83. doi: 10.2217/fmb-2018-0316. Epub 2019 Jan 15. 74(5):1323-1326. doi: 10.1093/jac/dky569. 74(3):639-644. doi: 10.1093/jac/dky493. 70(5):1466-72. doi: 10.1093/jac/dku542. Epub 2015 Jan 5. 31(2):e00079-17. doi: 10.1128/CMR.00079-17. 8: Zeiser ET, Becka SA, Barnes MD, Taracila MA, LiPuma JJ, Papp-Wallace KM. Resurrecting Old β-Lactams: Potent Inhibitory Activity of Temocillin against Multidrug-Resistant Burkholderia Species Isolates from the United States. Antimicrob Agents Chemother. 2019 Mar 27;63(4):e02315-18. doi: 10.1128/AAC.02315-18.
合成参考文献
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